Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules
Multi-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimodal and narrow size distributions with moderate di...
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2020-01-01
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Series: | Pharmaceutics |
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Online Access: | https://www.mdpi.com/1999-4923/12/1/80 |
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author | Cecilia B. Michalowski Marcelo D. Arbo Louise Altknecht Andréia N. Anciuti Angélica S. G. Abreu Luciana M. R. Alencar Adriana R. Pohlmann Solange C. Garcia Sílvia S. Guterres |
author_facet | Cecilia B. Michalowski Marcelo D. Arbo Louise Altknecht Andréia N. Anciuti Angélica S. G. Abreu Luciana M. R. Alencar Adriana R. Pohlmann Solange C. Garcia Sílvia S. Guterres |
author_sort | Cecilia B. Michalowski |
collection | DOAJ |
description | Multi-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimodal and narrow size distributions with moderate dispersity (laser diffraction and dynamic light scattering). Zeta potential was inverted from −14.3 mV [LNC-Fur(0,5)] to +18.3 mV after chitosan coating. Transmission electron microscopy and atomic force microscopy showed spherical structures corroborating the nanometric diameter of the nanocapsules. Regarding the systolic pressure, on the first day, the formulations showed antihypertensive effect and a longer effect than the respective drug solutions. When both drugs were associated, the anti-hypertensive effect was prolonged. On the fifth day, a time effect reduction was observed for all treatments, except for the nanocapsule formulation containing both drugs [Capt(0.5)-Zn(25)-MLNC-Fur(0.45)]. For diastolic pressure, only Capt(0.5)-Zn(25)-MLNC-Fur(0.45) presented a significant difference (<i>p</i> < 0.05) on the first day. On the fifth day, both Capt(0.5)-MLNC-Fur(0.45) and Capt(0.5)-Zn(25)-MLNC-Fur(0.45) had an effect lasting up to 24 h. The analysis of early kidney damage marker showed a potential protection in renal function by Capt(0.5)-Zn(25)-MLNC-Fur(0.45). In conclusion, the formulation Capt(0.5)-Zn(25)-MLNC-Fur(0.45) proved to be suitable for hypertension treatment envisaging an important innovation. |
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issn | 1999-4923 |
language | English |
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spelling | doaj.art-90ae1a1c2cff474685208c68dbfd9ced2022-12-22T04:01:19ZengMDPI AGPharmaceutics1999-49232020-01-011218010.3390/pharmaceutics12010080pharmaceutics12010080Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core NanocapsulesCecilia B. Michalowski0Marcelo D. Arbo1Louise Altknecht2Andréia N. Anciuti3Angélica S. G. Abreu4Luciana M. R. Alencar5Adriana R. Pohlmann6Solange C. Garcia7Sílvia S. Guterres8Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegr 90610-000, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegr 90610-000, BrazilLaboratório de Toxicologia (LATOX), Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegre 90610-000, BrazilInstituto de Ciências Básicas da Saúde, Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul, Rua Ramiro Barcelos, 2600 Anexo, Porto Alegre 90035-003, BrazilLaboratório de Microscopia Avançada, Departamento de Física, Universidade Federal do Ceara, Campus do Pici, Fortaleza 60455-900, BrazilLaboratório de Microscopia Avançada, Departamento de Física, Universidade Federal do Ceara, Campus do Pici, Fortaleza 60455-900, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegr 90610-000, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegr 90610-000, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Porto Alegr 90610-000, BrazilMulti-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimodal and narrow size distributions with moderate dispersity (laser diffraction and dynamic light scattering). Zeta potential was inverted from −14.3 mV [LNC-Fur(0,5)] to +18.3 mV after chitosan coating. Transmission electron microscopy and atomic force microscopy showed spherical structures corroborating the nanometric diameter of the nanocapsules. Regarding the systolic pressure, on the first day, the formulations showed antihypertensive effect and a longer effect than the respective drug solutions. When both drugs were associated, the anti-hypertensive effect was prolonged. On the fifth day, a time effect reduction was observed for all treatments, except for the nanocapsule formulation containing both drugs [Capt(0.5)-Zn(25)-MLNC-Fur(0.45)]. For diastolic pressure, only Capt(0.5)-Zn(25)-MLNC-Fur(0.45) presented a significant difference (<i>p</i> < 0.05) on the first day. On the fifth day, both Capt(0.5)-MLNC-Fur(0.45) and Capt(0.5)-Zn(25)-MLNC-Fur(0.45) had an effect lasting up to 24 h. The analysis of early kidney damage marker showed a potential protection in renal function by Capt(0.5)-Zn(25)-MLNC-Fur(0.45). In conclusion, the formulation Capt(0.5)-Zn(25)-MLNC-Fur(0.45) proved to be suitable for hypertension treatment envisaging an important innovation.https://www.mdpi.com/1999-4923/12/1/80lipid-core nanocapsulesantihypertensivesurface-functionalizationcaptoprilfurosemidetoxicityoral drug delivery |
spellingShingle | Cecilia B. Michalowski Marcelo D. Arbo Louise Altknecht Andréia N. Anciuti Angélica S. G. Abreu Luciana M. R. Alencar Adriana R. Pohlmann Solange C. Garcia Sílvia S. Guterres Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules Pharmaceutics lipid-core nanocapsules antihypertensive surface-functionalization captopril furosemide toxicity oral drug delivery |
title | Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules |
title_full | Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules |
title_fullStr | Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules |
title_full_unstemmed | Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules |
title_short | Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules |
title_sort | oral treatment of spontaneously hypertensive rats with captopril surface functionalized furosemide loaded multi wall lipid core nanocapsules |
topic | lipid-core nanocapsules antihypertensive surface-functionalization captopril furosemide toxicity oral drug delivery |
url | https://www.mdpi.com/1999-4923/12/1/80 |
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